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Literature summary for 2.7.11.22 extracted from

  • Liu, M.; Choi, S.; Cuny, G.D.; Ding, K.; Dobson, B.C.; Glicksman, M.A.; Auerbach, K.; Stein, R.L.
    Kinetic studies of Cdk5/p25 kinase: phosphorylation of tau and complex inhibition by two prototype inhibitors (2008), Biochemistry, 47, 8367-8377.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
p25
-
Homo sapiens

Application

Application Comment Organism
medicine causal role in Alzheimer's disease Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(5-cyclobutyl-thiazol-2-yl)-3-isoquinolin-5-yl-urea competitive inhibitor Homo sapiens
AMP competitive inhibitor Homo sapiens
H1PAla noncompetitive inhibitor Homo sapiens
H1PPO4 noncompetitive inhibitor Homo sapiens
N4-(6-aminopyrimidin-4-yl)-sulfanilamide competitive inhibitor Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.017
-
ATP in 20 mM MOPS (pH 7.5), at 30°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + histone H1-derived peptide
-
Homo sapiens ADP + histone H1-derived peptide phosphate
-
?
ATP + protein tau
-
Homo sapiens ADP + protein tau phosphate
-
?

Synonyms

Synonyms Comment Organism
cdk5/p25 kinase
-
Homo sapiens

Turnover Number [1/s]

Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
0.28
-
ATP in 20 mM MOPS (pH 7.5), at 30°C Homo sapiens

Cofactor

Cofactor Comment Organism Structure
ATP
-
Homo sapiens
cyclin
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0036
-
in 20 mM MOPS (pH 7.5), at 30°C Homo sapiens N4-(6-aminopyrimidin-4-yl)-sulfanilamide